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Design, synthesis, and biological evaluation of novel human 5'-deoxy-5'-methylthioadenosine phosphorylase (MTAP) substrates |
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| Authors: | Kung Pei-Pei Zehnder Luke R Meng Jerry J Kupchinsky Stanley W Skalitzky Donald J Johnson M Catherine Maegley Karen A Ekker Anne Kuhn Leslie A Rose Peter W Bloom Laura A |
| Institution: | Pfizer Global Research and Development-La Jolla, San Diego, CA 92121, USA. peipei.kung@pfizer.com |
| Abstract: | The structure-based design, chemical synthesis, and biological evaluation of novel MTAP substrates are described. These compounds incorporate various C5'-moieties and are shown to have different k(cat)/K(m) values compared with the natural MTAP substrate (MTA). |
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